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1.发明公开EFFICIENT ENANTIOSELECTIVE ADDITION REACTION USING AN ORGANOZINC REAGENT 失效对映选择性ADDITIONS反应中，用有机锌试剂
公开(公告)号：EP0981520A1
公开(公告)日：2000-03-01
申请号：EP98922084.3
申请日：1998-05-12
申请人： MERCK & CO., INC.
IPC分类号： C07D265/18
CPC分类号： C07D265/18 , C07B2200/07 , C07C213/08 , C07C215/68 , C07C215/70
摘要： An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.
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2.发明授权EFFICIENT ENANTIOSELECTIVE ADDITION REACTION USING AN ORGANOZINC REAGENT 失效对映选择性ADDITIONS反应中，用有机锌试剂
公开(公告)号：EP0981520B1
公开(公告)日：2004-07-07
申请号：EP98922084.3
申请日：1998-05-12
申请人： MERCK & CO., INC.
IPC分类号： C07D265/18
CPC分类号： C07D265/18 , C07B2200/07 , C07C213/08 , C07C215/68 , C07C215/70
摘要： An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.
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3.发明授权PROCESS FOR ENHANCING THE OPTICAL PURITY OF 2R- 1-HYDROXY- 1-TRIFLUOROMETHYL- 3-CYCLOPROPYLPROPYN-2YL] -4-CHLOROANILINE 有权PROCESS FOR改进光学2R [1-羟基-1-三氟甲基-3- cyclopropylpropyn -2-基] -4-氯苯胺的纯度
公开(公告)号：EP1017666B1
公开(公告)日：2003-11-05
申请号：EP98942339.7
申请日：1998-09-01
申请人： MERCK & CO., INC.
发明人： CHEN, Cheng, Yi , REIDER, Paul, J. , GRABOWSKI, Edward, J., J. , TAN, Lushi , TILLYER, Richard, D.
IPC分类号： C07C209/88 , C07C211/46 , C07C211/52 , C07C213/10 , C07B57/00
CPC分类号： C07C213/10 , C07B2200/07 , C07C2601/02 , C07C215/70
摘要： A process for enhancing the purity of 2R-[1-hydroxy- 1-trifluoromethyl- 3-cyclopropylpropyn-2-yl] -4-chloroaniline comprising the formation of an acid addition salt which is capable of rejecting the racemate in the selected organic solvent.
摘要翻译： 一种用于增强2R-的纯度工艺[1-羟基-1-三氟甲基-3- cyclopropylpropyn -2-基] -4-氯苯胺，包括酸加成盐的所有其能够在所选择的有机溶剂中拒绝所述外消旋物的形成 ，
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4.发明公开PROCESS FOR ENHANCING THE OPTICAL PURITY OF 2R- 1-HYDROXY- 1-TRIFLUOROMETHYL- 3-CYCLOPROPYLPROPYN-2YL] -4-CHLOROANILINE 有权PROCESS FOR改进光学2R [1-羟基-1-三氟甲基-3- cyclopropylpropyn -2-基] -4-氯苯胺的纯度
公开(公告)号：EP1017666A1
公开(公告)日：2000-07-12
申请号：EP98942339.7
申请日：1998-09-01
申请人： MERCK & CO., INC.
发明人： CHEN, Cheng, Yi , REIDER, Paul, J. , GRABOWSKI, Edward, J., J. , TAN, Lushi , TILLYER, Richard, D.
IPC分类号： C07C209/88 , C07C211/46 , C07C211/52
CPC分类号： C07C213/10 , C07B2200/07 , C07C2601/02 , C07C215/70
摘要： A process for enhancing the purity of 2R-[1-hydroxy- 1-trifluoromethyl- 3-cyclopropylpropyn-2-yl] -4-chloroaniline comprising the formation of an acid addition salt which is capable of rejecting the racemate in the selected organic solvent.
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公开(公告)号：EP0973737A1
公开(公告)日：2000-01-26
申请号：EP98903459.0
申请日：1998-01-06
申请人： MERCK & CO., INC.
发明人： CHEN, Cheng, Yi , XU, Feng , TILLYER, Richard, D. , ZHAO, Dalian
IPC分类号： C07D205/04 , C07D209/44 , C07D211/14 , C07D221/04 , C07D295/088 , C07D295/092 , C07D295/096
CPC分类号： C07D221/14 , C07B2200/07 , C07C2602/08 , C07D205/04 , C07D209/44 , C07D295/092 , C07D295/096
摘要： An efficient method for the quantitative preparation and isolation of a compound of formula (I) or its enantiomer, a chiral mediator used in enantioselective synthesis.
摘要翻译： 用于定量制备和分离式（I）化合物或其对映异构体的有效方法，其用于对映选择性合成中使用的手性介体。
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